Abrocitinib

JAK1抑制剂(IC50=0.029µM)；对JAK1具有选择性，而对JAK2、JAK3和TYK2则无选择性（IC50s分别为0.803、>10和1.253µM），对1µM浓度的40种激酶亦有选择性；在分离的人全血中，可抑制IFN-α、IL-21或IL-27诱导的STAT3磷酸化（IC50s分别为0.189、0.511和0.271µM）和IFN-γ诱导的STAT1磷酸化（IC50=0.163µM）；在1、5和15mg/kg剂量下，可减轻佐剂诱发性关节炎大鼠模型中的爪水肿。A JAK1 inhibitor (IC50 = 0.029 µM); selective for JAK1 over JAK2, JAK3, and TYK2 (IC50s = 0.803, >10, and 1.253 µM, respectively) and a panel of 40 kinases at 1 µM; inhibits IFN-α-, IL-21-, or IL-27-induced phosphorylation of STAT3 (IC50s = 0.189, 0.511, and 0.271 µM, respectively) and IFN-γ-induced phosphorylation of STAT1 (IC50 = 0.163 µM) in isolated human whole blood; reduces paw edema in a rat model of adjuvant-induced arthritis at 1, 5, and 15 mg/kg.分子式C14H21N5O2S分子量323.4CN([C@H]1C[C@H](C1)NS(CCC)(=O)=O)C2=C3C(NC=C3)=NC=N2